Pharmaceutical compositions for neuroprotection containing arylcyclohexylamines

Abstract

PCT No. PCT/FR89/00596 Sec. 371 Date Jun. 21, 1990 Sec. 102(e) Date Jun. 21, 1990 PCT Filed Nov. 20, 1989 PCT Pub. No. WO90/05524 PCT Pub. Date May 31, 1990.The invention relates to pharmaceutical compositions for neuroprotection containing arylcyclohexylamines. These compositions comprise an arylcyclohexylamine in accordance with the formulas: <IMAGE> (I) <IMAGE> (II) in which: R1 represents <IMAGE> with R4 being a hydrogen atom, a fluorine atom, an iodine atom or a methyl radical, R2 stands for a hydrogen atom, the radical OH or the radical CH3 and R3 stands for hydrogen atom or the radical CH2R5 with R5 representing H, OH, Cl, Br or CH3COO, provided that R2 and R3 are not both a hydrogen atom, or an addition salt to a pharmaceutically acceptable acid of said arylcyclohexylamine.

What is claimed is: 
     
       1. A method of treating a human being to prevent cerebral attacks which occur during acute ailments or diseases and to protect the brain against neuronal loss or to extend neuronal life in the cerebral cortex, the hippocampus and the cerebellum by administering to a human being in need thereof an effective amount of a neuroprotective medicament including as its active ingredient an arylcyclohexylamine in accordance with the formulas: ##STR66## in which: R 1  represents ##STR67##  with R 4  being a hydrogen atom, a fluorine atom, an iodine atom or a methyl radical, R 2  a hydrogen atom, the OH radical or the CH 3  radical and R 3  a hydrogen atom or the radical CH 2  R 5  with R 5  representing H, OH, Cl, Br or CH 3  COO, provided that R 2  and R 3  are not both a hydrogen atom, or an addition salt to a pharmaceutically acceptable acid of said arylcyclohexylamine. 
     
     
       2. A method according to claim 1, characterized in that the arylcyclohexylamine is in accordance with the formula: ##STR68## in which R 3  stands for the methyl radical or the radical CH 2  R 5  with R 5  representing OH or CH 3  COO and R 4  stands for a hydrogen atom. 
     
     
       3. A method according to claim 1, characterized in that the arylcyclohexylamine is in accordance with the formula: ##STR69## in which R 2  is the methyl radical, R 3  the radical CH 2  R 5  with R 5  representing OH and R 4  is a fluorine atom. 
     
     
       4. A method according to claim 1, characterized in that the arylcyclohexylamine is in accordance with formula: ##STR70## 
     
     
       5. A method according to claim 1, characterized in that the arylcyclohexylamine is in accordance with formula: ##STR71## in which R 2  is the methyl radical. 
     
     
       6. A method according to claim 1, characterized in that the arylcyclohexylamine is in accordance with the formula: ##STR72## in which R 3  is the CH 2  R 5  radical with R 5  representing OH or Cl. 
     
     
       7. A method according to claim 1, characterized in that the arylcyclohexylamine is in accordance with the formula: ##STR73## in which R 2  is the methyl radical and R 3  the radical CH 2  OH. 
     
     
       8. A method according to claim 1, characterized in that the arylcyclohexylamine is in accordance with the formula: ##STR74## in which CH 3  is in the cis position with respect to the piperidine. 
     
     
       9. A method according to any one of the claims 1, 3, 4, 5 and 7, characterized in that R 2  is in the ortho position. 
     
     
       10. A method of treating a human being to prevent cerebral attacks which occur during acute ailments or diseases and to protect the brain against neuronal loss or to extend neuronal life in the cerebral cortex, the hippocampus and the cerebellum by administering to a human being in need thereof an effective amount of a neuroprotective medicament including as its active ingredient the compound TCP of formula: ##STR75##